EA200800668A1 - Производные пиразина и их применение в качестве ингибиторов pi3k - Google Patents

Производные пиразина и их применение в качестве ингибиторов pi3k

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Publication number
EA200800668A1
EA200800668A1 EA200800668A EA200800668A EA200800668A1 EA 200800668 A1 EA200800668 A1 EA 200800668A1 EA 200800668 A EA200800668 A EA 200800668A EA 200800668 A EA200800668 A EA 200800668A EA 200800668 A1 EA200800668 A1 EA 200800668A1
Authority
EA
Eurasian Patent Office
Prior art keywords
pyrazine
derivatives
application
diseases
pi3k inhibitors
Prior art date
Application number
EA200800668A
Other languages
English (en)
Other versions
EA015937B1 (ru
Inventor
Паскаль Гайяр
Анна Кваттропани
Винсэн Помель
Томас Рюкле
Ясна Кличич
Деннис Черч
Original Assignee
Лаборатуар Сероно С.А.
Priority date (The priority date is an assumption and is not a legal conclusion. Google has not performed a legal analysis and makes no representation as to the accuracy of the date listed.)
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Publication date
Application filed by Лаборатуар Сероно С.А. filed Critical Лаборатуар Сероно С.А.
Publication of EA200800668A1 publication Critical patent/EA200800668A1/ru
Publication of EA015937B1 publication Critical patent/EA015937B1/ru

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    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D241/00Heterocyclic compounds containing 1,4-diazine or hydrogenated 1,4-diazine rings
    • C07D241/36Heterocyclic compounds containing 1,4-diazine or hydrogenated 1,4-diazine rings condensed with carbocyclic rings or ring systems
    • C07D241/38Heterocyclic compounds containing 1,4-diazine or hydrogenated 1,4-diazine rings condensed with carbocyclic rings or ring systems with only hydrogen or carbon atoms directly attached to the ring nitrogen atoms
    • C07D241/40Benzopyrazines
    • C07D241/44Benzopyrazines with hetero atoms or with carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, e.g. ester or nitrile radicals, directly attached to carbon atoms of the hetero ring
    • AHUMAN NECESSITIES
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    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00Medicinal preparations containing organic active ingredients
    • A61K31/33Heterocyclic compounds
    • A61K31/395Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
    • A61K31/495Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with two or more nitrogen atoms as the only ring heteroatoms, e.g. piperazine or tetrazines
    • A61K31/498Pyrazines or piperazines ortho- and peri-condensed with carbocyclic ring systems, e.g. quinoxaline, phenazine
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Abstract

Настоящее изобретение относится к производным пиразина формулы (I)в частности, для лечения и/или профилактики аутоиммунных нарушений и/или воспалительных заболеваний, сердечно-сосудистых заболеваний, нейродегенеративных заболеваний, бактериальных и вирусных инфекций, заболеваний почек, агрегации тромбоцитов, рака, нарушений при трансплантации, отторжения трансплантата или повреждений легких.
EA200800668A 2005-08-26 2006-08-25 Производные пиразина и их применение в качестве ингибиторов pi3k EA015937B1 (ru)

Applications Claiming Priority (3)

Application Number Priority Date Filing Date Title
US71187305P 2005-08-26 2005-08-26
EP05107838 2005-08-26
PCT/EP2006/065688 WO2007023186A1 (en) 2005-08-26 2006-08-25 Pyrazine derivatives and use as pi3k inhibitors

Publications (2)

Publication Number Publication Date
EA200800668A1 true EA200800668A1 (ru) 2008-08-29
EA015937B1 EA015937B1 (ru) 2011-12-30

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Application Number Title Priority Date Filing Date
EA200800668A EA015937B1 (ru) 2005-08-26 2006-08-25 Производные пиразина и их применение в качестве ингибиторов pi3k

Country Status (18)

Country Link
US (3) US8071597B2 (ru)
EP (2) EP1917252B1 (ru)
JP (1) JP5226513B2 (ru)
KR (1) KR20080049767A (ru)
CN (1) CN101296909B (ru)
AU (1) AU2006283846B2 (ru)
BR (1) BRPI0615233A2 (ru)
CA (1) CA2618479C (ru)
EA (1) EA015937B1 (ru)
EC (1) ECSP088215A (ru)
ES (1) ES2456000T3 (ru)
HK (1) HK1123296A1 (ru)
IL (1) IL189737A (ru)
MX (1) MX2008002723A (ru)
NZ (1) NZ565749A (ru)
UA (1) UA100358C2 (ru)
WO (1) WO2007023186A1 (ru)
ZA (1) ZA200801822B (ru)

Families Citing this family (81)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
KR20140033237A (ko) * 2005-10-07 2014-03-17 엑셀리시스, 인코포레이티드 포스파티딜이노시톨 3-키나아제 억제제 및 이의 사용 방법
US8217042B2 (en) 2005-11-11 2012-07-10 Zentaris Gmbh Pyridopyrazines and their use as modulators of kinases
EP1790342A1 (de) 2005-11-11 2007-05-30 Zentaris GmbH Pyridopyrazin-Derivate und deren Verwendung als Modulatoren der Signaltransduktionswege
JP2010500994A (ja) 2006-08-16 2010-01-14 エグゼリクシス, インコーポレイテッド Pi3kおよびmekモジュレーターを使用する方法
EA200970783A1 (ru) * 2007-02-22 2010-04-30 Мерк Сероно С.А. Соединения хиноксалина и их применение
US7705018B2 (en) 2007-03-23 2010-04-27 Amgen Inc. Substituted quinolines and their uses in treatment of inflammatory and related conditions
US8481001B2 (en) * 2007-04-11 2013-07-09 Exelixis, Inc. Combination therapies comprising quinoxaline inhibitors of P13K-alpha for use in the treatment of cancer
WO2009017838A2 (en) * 2007-08-01 2009-02-05 Exelixis, Inc. Combinations of jak-2 inhibitors and other agents
CN101918531B (zh) 2007-11-20 2013-06-12 3M创新有限公司 环境取样制品和方法
WO2009082667A1 (en) 2007-12-21 2009-07-02 3M Innovative Properties Company Microbiological systems and methods of fluid sample analysis
WO2009155527A2 (en) * 2008-06-19 2009-12-23 Progenics Pharmaceuticals, Inc. Phosphatidylinositol 3 kinase inhibitors
ES2463676T3 (es) 2008-11-10 2014-05-28 Kyowa Hakko Kirin Co., Ltd. Inhibidor de la producción de quinurenina
US20120121515A1 (en) 2009-03-13 2012-05-17 Lenny Dang Methods and compositions for cell-proliferation-related disorders
CN102448951B (zh) 2009-04-06 2017-05-10 安吉奥斯医药品有限公司 丙酮酸激酶m2调节剂、治疗组合物和相关使用方法
DK2427441T3 (en) 2009-05-04 2017-03-20 Agios Pharmaceuticals Inc PKM2 Activators for use in the treatment of cancer
EP2448581B1 (en) 2009-06-29 2016-12-07 Agios Pharmaceuticals, Inc. Therapeutic compositions and related methods of use
TWI649313B (zh) * 2009-06-29 2019-02-01 阿吉歐斯製藥公司 治療化合物及組成物
US9649331B2 (en) 2009-08-27 2017-05-16 Ara Medical Llc Sprayable polymers as adhesion barriers
EP2473504B1 (en) 2009-09-03 2015-02-25 Bioenergenix Heterocyclic compounds for the inhibition of pask
DE102009049679A1 (de) 2009-10-19 2011-04-21 Merck Patent Gmbh Pyrazolopyrimidinderivate
WO2011050210A1 (en) 2009-10-21 2011-04-28 Agios Pharmaceuticals, Inc. Methods and compositions for cell-proliferation-related disorders
EP2525790B1 (en) 2009-10-21 2020-05-27 Agios Pharmaceuticals, Inc. Methods and compositions for cell-proliferation-related disorders
CN102713616B (zh) 2009-12-30 2014-10-15 3M创新有限公司 微生物检测制品
GB201007286D0 (en) 2010-04-30 2010-06-16 Astex Therapeutics Ltd New compounds
TWI535442B (zh) * 2010-05-10 2016-06-01 Kyowa Hakko Kirin Co Ltd A nitrogen-containing heterocyclic compound having an action of inhibiting the production of canine erythritine
CN102311396B (zh) 2010-07-05 2015-01-07 暨南大学 一种吡嗪类衍生物和其制备方法及在制药中的应用
EA201390582A1 (ru) 2010-10-20 2013-09-30 Мерк Сероно С.А. Женева Способ получения замещенных n-(3-аминохиноксалин-2-ил)сульфонамидов и их промежуточных n-(3-хлорхиноксалин-2-ил)сульфонамидов
DE102010048800A1 (de) 2010-10-20 2012-05-10 Merck Patent Gmbh Chinoxalinderivate
DE102010049595A1 (de) 2010-10-26 2012-04-26 Merck Patent Gmbh Chinazolinderivate
CA2821975A1 (en) 2010-12-17 2012-06-21 Shunqi Yan N-(4-(azetidine-1-carbonyl)phenyl)-(hetero-) arylsulfonamide derivatives as pyruvate kinase m2 pkm2 modulators
JP6092118B2 (ja) 2010-12-21 2017-03-08 アジオス ファーマシューティカルズ, インコーポレイテッド ニ環式pkm2活性化剤
TWI549947B (zh) 2010-12-29 2016-09-21 阿吉歐斯製藥公司 治療化合物及組成物
EP2681207B1 (en) * 2011-03-02 2016-12-28 Bioenergenix Heterocyclic compounds for the inhibition of pask
CA2832099C (en) 2011-04-05 2019-07-09 Sloan-Kettering Institute For Cancer Research Hsp90 inhibitors
EP2518071A1 (en) * 2011-04-29 2012-10-31 Almirall, S.A. Imidazopyridine derivatives as PI3K inhibitors
EP2518070A1 (en) 2011-04-29 2012-10-31 Almirall, S.A. Pyrrolotriazinone derivatives as PI3K inhibitors
AU2012250690B2 (en) 2011-05-03 2017-06-08 Agios Pharmaceuticals, Inc Pyruvate kinase activators for use in therapy
FI3406251T3 (fi) 2011-05-03 2024-02-21 Agios Pharmaceuticals Inc Pyruvaattikinaasin aktivaattoreita terapeuttista käyttöä varten
CN102827073A (zh) 2011-06-17 2012-12-19 安吉奥斯医药品有限公司 治疗活性组合物和它们的使用方法
CN102827170A (zh) 2011-06-17 2012-12-19 安吉奥斯医药品有限公司 治疗活性组合物和它们的使用方法
CN102389574A (zh) * 2011-09-21 2012-03-28 谢钰容 Itpka基因及其表达蛋白在制备及筛选抗癌药物中的应用
GB201118654D0 (en) * 2011-10-28 2011-12-07 Astex Therapeutics Ltd New compounds
GB201118656D0 (en) 2011-10-28 2011-12-07 Astex Therapeutics Ltd New compounds
GB201118652D0 (en) 2011-10-28 2011-12-07 Astex Therapeutics Ltd New compounds
US9067923B2 (en) 2011-11-09 2015-06-30 Kyowa Hakko Kirin Co., Ltd. Substituted quinoxalines
US9949979B2 (en) 2011-12-15 2018-04-24 Novartis Ag Use of inhibitors of the activity or function of PI3K
KR101362417B1 (ko) 2012-01-03 2014-02-14 한국과학기술원 PI3Kβ 저해활성을 갖는 아미노피리미딘계 유도체, 이를 포함하는 PI3Kβ 저해제 조성물 및 그 제조방법
DK2800743T3 (en) 2012-01-06 2018-06-14 Agios Pharmaceuticals Inc THERAPEUTIC ACTIVE RELATIONS AND PROCEDURES FOR USE THEREOF
US9474779B2 (en) 2012-01-19 2016-10-25 Agios Pharmaceuticals, Inc. Therapeutically active compositions and their methods of use
GB201209613D0 (en) 2012-05-30 2012-07-11 Astex Therapeutics Ltd New compounds
CN104640862B (zh) * 2012-07-27 2017-02-15 和记黄埔医药(上海)有限公司 新的杂芳基和杂环化合物、其组合物及方法
WO2014015523A1 (en) * 2012-07-27 2014-01-30 Hutchison Medipharma Limited Novel heteroaryl and heterocycle compounds, compositions and methods
US9487526B2 (en) 2012-08-13 2016-11-08 Takeda Pharmaceutical Company Limited Quinoxaline derivatives as GPR6 modulators
CA2888360A1 (en) 2012-10-15 2014-04-24 Agios Pharmaceuticals, Inc. Therapeutic compounds and compositions
WO2014060432A1 (en) * 2012-10-16 2014-04-24 Almirall, S.A. Pyrrolotriazinone derivatives as pi3k inhibitors
CN105377837B (zh) 2013-05-14 2017-08-04 活跃生物技术有限公司 用作s100‑抑制剂的n‑(杂芳基)磺酰胺衍生物
US9579324B2 (en) 2013-07-11 2017-02-28 Agios Pharmaceuticals, Inc Therapeutically active compounds and their methods of use
WO2015003355A2 (en) 2013-07-11 2015-01-15 Agios Pharmaceuticals, Inc. Therapeutically active compounds and their methods of use
AU2014287121B2 (en) 2013-07-11 2018-11-15 Agios Pharmaceuticals, Inc. 2,4- or 4,6-diaminopyrimidine compounds as IDH2 mutants inhibitors for the treatment of cancer
WO2015003360A2 (en) 2013-07-11 2015-01-15 Agios Pharmaceuticals, Inc. Therapeutically active compounds and their methods of use
US20150031627A1 (en) 2013-07-25 2015-01-29 Agios Pharmaceuticals, Inc Therapeutically active compounds and their methods of use
CN103739525B (zh) * 2013-12-30 2016-05-25 京博农化科技股份有限公司 一种取代苯磺酰氯的制备方法
JP6526034B2 (ja) 2014-02-14 2019-06-05 武田薬品工業株式会社 Gpr6のピリドピラジンモジュレーター
CN106255498B (zh) 2014-03-14 2020-06-26 阿吉奥斯制药公司 治疗活性化合物的药物组合物
MX2016012368A (es) 2014-03-26 2017-02-23 Astex Therapeutics Ltd Combinaciones de un inhibidor del factor de crecimiento de fibroblasto (fgfr) y un inhibidor del receptor del factor de crecimiento 1 similar a insulina (igf1r).
JO3512B1 (ar) 2014-03-26 2020-07-05 Astex Therapeutics Ltd مشتقات كينوكسالين مفيدة كمعدلات لإنزيم fgfr كيناز
KR102479693B1 (ko) 2014-03-26 2022-12-22 아스텍스 테라퓨틱스 리미티드 조합물
KR20170010369A (ko) * 2014-05-27 2017-01-31 알미랄, 에스.에이. 병용물
JOP20200201A1 (ar) 2015-02-10 2017-06-16 Astex Therapeutics Ltd تركيبات صيدلانية تشتمل على n-(3.5- ثنائي ميثوكسي فينيل)-n'-(1-ميثيل إيثيل)-n-[3-(ميثيل-1h-بيرازول-4-يل) كينوكسالين-6-يل]إيثان-1.2-ثنائي الأمين
US10478494B2 (en) 2015-04-03 2019-11-19 Astex Therapeutics Ltd FGFR/PD-1 combination therapy for the treatment of cancer
US10273246B2 (en) 2015-05-18 2019-04-30 University Of Utah Research Foundation Methods and compositions of substituted 5H-[1,2,5] oxadiazolo [3′,4′:5,6] pyrazino[2,3-B] indole analogs as inhibitors of β-catenin/T-cell factor protein-protein interactions
ES2959690T3 (es) 2015-06-11 2024-02-27 Agios Pharmaceuticals Inc Procedimientos de uso de activadores de piruvato cinasa
WO2017050865A1 (en) 2015-09-23 2017-03-30 Janssen Pharmaceutica Nv Bi-heteroaryl substituted 1,4-benzodiazepines and uses thereof for the treatment of cancer
SI3353177T1 (sl) 2015-09-23 2020-08-31 Janssen Pharmaceutica Nv Triciklični heterocikli za zdravljenje raka
CA3002067C (en) 2015-10-15 2023-11-28 Agios Pharmaceuticals, Inc. Combination therapy for treating malignancies
SG10202111435UA (en) 2015-10-15 2021-12-30 Les Laboratoires Servier Sas Combination therapy for treating malignancies
US20200223839A1 (en) * 2017-07-09 2020-07-16 Jiangsu Yingkebeita Yiyaokeji Co. Ltd Fluoro-containing compounds, use and preparation thereof
IL277071B1 (en) 2018-03-08 2024-03-01 Incyte Corp Aminopyrizine diol compounds as PI3K–y inhibitors
US10980788B2 (en) 2018-06-08 2021-04-20 Agios Pharmaceuticals, Inc. Therapy for treating malignancies
WO2023144711A1 (en) 2022-01-27 2023-08-03 Pi Industries Ltd. 1,2,3-triazole carbonyl sulfonylamide compounds and use thereof
CN114573517B (zh) * 2022-03-10 2024-04-26 新乡医学院 一种喹喔啉类化合物及其制备方法与应用

Family Cites Families (10)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US6667300B2 (en) * 2000-04-25 2003-12-23 Icos Corporation Inhibitors of human phosphatidylinositol 3-kinase delta
IL152275A0 (en) * 2000-04-25 2003-05-29 Icos Corp Inhibitors of human phosphatidyl-inositol 3-kinase delta
CA2407593C (en) * 2000-04-27 2011-01-11 Yamanouchi Pharmaceutical Co. Ltd. Fused heteroaryl derivatives
CA2493843C (en) 2002-07-10 2012-04-17 Applied Research Systems Ars Holding N.V. Azolidinone-vinyl fused-benzene derivatives
EP1581529A1 (en) 2002-12-20 2005-10-05 Warner-Lambert Company Benzoxazines and derivatives thereof as inhibitors of pi3ks
GB0305152D0 (en) 2003-03-06 2003-04-09 Novartis Ag Organic compounds
GB0320197D0 (en) 2003-08-28 2003-10-01 Novartis Ag Organic compounds
US7592340B2 (en) * 2003-12-04 2009-09-22 Vertex Pharmaceuticals Incorporated Quinoxalines useful as inhibitors of protein kinases
JP2006137723A (ja) * 2004-11-15 2006-06-01 Kyowa Hakko Kogyo Co Ltd スルホンアミド誘導体
RU2453540C2 (ru) * 2005-04-21 2012-06-20 Лаборатуар Сероно С.А. 2,3-замещенные пиразинсульфонамиды в качестве ингибиторов crth2

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